A class of pyridazinone derivatives as near-infrared optical probes in fluorescence microscopy images was designed. The design strategy consisted of the stepwise extension and modification of pyridazinone by expansion of the electron-donating moiety to a larger π-conjugated system and anchoring a subcellular directing group such as triphenylphosphine or morpholine. All the desired products were successfully applied in cell imaging with high subcellular colocalization. Furthermore, these fluorescent probes showed excellent performance in mouse-brain imaging.

In this study we designed a series of proteasome inhibitors using pyridazinone as initial scaffold, and extended the structure with rational design by computer aided drug design (CADD). Two different synthetic routes were explored and the biological evaluation of the phthalazinone derivatives was investigated. Most importantly, electron positive triphenylphosphine group was first introduced in the structure of proteasome inhibitors and potent inhibition was achieved. As 6c was the most potent inhibitor of proteasome, we examined the structure–activity relationship (SAR) of 6c analogs.

We reported the synthesis, characterization and biological activity of several copper(II) Schiff base complexes, which exhibit high proteasome inhibitory activities with particular selectivity of β2 subunit. Structure–activity relationships information obtained from complex Na2[Cu(a4s1)] demonstrated that distinct bonding modes in β2 and β5 subunits determines its selectivity and potent inhibition for β2 subunit.

We reported the synthesis, characterization and biological activity of several copper(II) Schiff base complexes, which exhibit high proteasome inhibitory activities with particular selectivity of β2 subunit. Structure–activity relationships information obtained from complex Na2[Cu(a4s1)] demonstrated that distinct bonding modes in β2 and β5 subunits determines its selectivity and potent inhibition for β2 subunit.